Imidazo[4,5-b]pyridine derivatives of potential tuberculostatic activity. Part 1: Synthesis and quantitative structure-activity relationships.

New derivatives of imidazo[4,5-b]pyridine and 9H-dipyrido-[1,2-a:3',2'-d]imidazole were synthesized. Antibacterial activity against Mycobacterium tuberculosis of selected compounds was determined. These data were combined with the corresponding bioactivity data previously generated for two other series of imidazo[4,5-b]pyridines. Analysis of Quantitative Structure-Activity Relationships [QSAR] was carried out using nonempirical structural descriptors. Hydrophobicity of the agents studied was found decisive for their activity. A QSAR equation was derived allowing rational design of active derivatives.